SR-3677

Rho Kinase (ROCK-II) inhibitor CAS# 1072959-67-1

SR-3677

Catalog No. BCC4302----Order now to get a substantial discount!

Product Name & Size Price Stock
SR-3677:100mg $523.00 In stock
SR-3677:200mg $889.00 In stock
SR-3677:500mg $2092.00 In stock
SR-3677:1000mg $3661.00 In stock
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Quality Control of SR-3677

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Chemical structure

SR-3677

3D structure

Chemical Properties of SR-3677

Cas No. 1072959-67-1 SDF Download SDF
PubChem ID 25093235 Appearance Powder
Formula C22H24N4O4 M.Wt 408.45
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 43 mg/mL (105.28 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxine-3-carboxamide
SMILES CN(C)CCOC1=C(C=CC(=C1)C2=CNN=C2)NC(=O)C3COC4=CC=CC=C4O3
Standard InChIKey OQWZIAVXCYIZNN-UHFFFAOYSA-N
Standard InChI InChI=1S/C22H24N4O4/c1-26(2)9-10-28-20-11-15(16-12-23-24-13-16)7-8-17(20)25-22(27)21-14-29-18-5-3-4-6-19(18)30-21/h3-8,11-13,21H,9-10,14H2,1-2H3,(H,23,24)(H,25,27)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SR-3677

DescriptionPotent and selective Rho-kinase inhibitor (IC50 values are 3 and 56 nM for ROCK-II and ROCK-I respectively).

Protocol

Kinase Assay [1]
Assays are performed using the STK2 kinase system from Cisbio. 5 μL mixture of a 1 μM STK2 substrate and ATP (ROCK-I: 4 μM; ROCK-II: 20 μM) in STK-buffer is added to the wells. 20 nL of test compounds (SR-3677) is dispensed. Reaction is started by addition of 5 μL of 2.5 nM. ROCK-I or 0.5 nM ROCK-II in STK-buffer. After 4 h at RT the reaction is stopped by addition of 10 μL of 1x antibody and 62.5 nM Sa-XL in detection buffer[1].

References:
[1]. Feng Y, et al. Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem. 2008 Nov 13;51(21):6642-5.

SR-3677 Dilution Calculator

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SR-3677 Molarity Calculator

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Preparing Stock Solutions of SR-3677

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4483 mL 12.2414 mL 24.4828 mL 48.9656 mL 61.207 mL
5 mM 0.4897 mL 2.4483 mL 4.8966 mL 9.7931 mL 12.2414 mL
10 mM 0.2448 mL 1.2241 mL 2.4483 mL 4.8966 mL 6.1207 mL
50 mM 0.049 mL 0.2448 mL 0.4897 mL 0.9793 mL 1.2241 mL
100 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.4897 mL 0.6121 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on SR-3677

SR-3677 is a novel, potent and highly selective inhibitor of Rho Kinase (ROCK-II) with the IC50 value of ~0.3nM in enzyme and cell based assays [1].

SR-3677 has been reported to selectively inhibit the ROCK- II with the IC50 values of ~3nM, ~3nM, 56nM, 3.968μM,1.190μM and 7.491μM for ROCK-II,ppMLC, ROCK-I, PKA, MRCK and Akt1, respectively. In addition, SR-3677 has been shown several key binding elements that contribute to the high potency and selectivity in the docking assay. Furthermore, SR-3677 has been revealed to be efficacious in enhancing aqueous humor outflow and in target modulation in the pharmacology studies [1].

References:
[1] Feng Y1, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter T, Lograsso P. Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem. 2008 Nov 13;51(21):6642-5. doi: 10.1021/jm800986w. Epub 2008 Oct 4.

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References on SR-3677

Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.[Pubmed:18834107]

J Med Chem. 2008 Nov 13;51(21):6642-5.

The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC 50 of approximately 3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.

Description

SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM.

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